Process for the preparation of cyclo (asp-dphe-nmeval-arg-gly)

Details Process for the preparation of cyclo (asp-dphe-nmeval-arg-gly) Process for the preparation of cyclo (asp-dphe-nmeval-arg-gly)

C - Chemistry, Metallurgy

07

K

C07K 7/64 (2006.01) C07K 5/06 (2006.01) C07K 5/072 (2006.01) C07K 5/08 (2006.01) C07K 5/093 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2366694

The invention relates to a method for producing the cyclic pentapeptide cyclo- (Arg-Gly-Asp-DPhe-NMeVal) by cyclising a linear pentapeptide chosen from the group H-Arg(Pbf) -Gly-Asp(OBzl) -DPhe- NMeVal-OH, H-Gly-Asp(OBzl) -DPhe-NMeVal-Arg (Pbf)-OH, H-Asp(OBzl) -DPhe-NMeVal-Arg (Pbf)-Gly-OH, H-DPhe-NMeVal-Arg (Pbf)- Gly-Asp (OBzl)-OH or H-NMeVal-Arg (Pbf)-Gly-Asp (OBzl)-DPhe-OH, subsequently separating protective groups and optionally further converting into the physiologically unobjectionable salts thereof.

La présente invention a pour objet une méthode de production de pentapeptide cyclique, de type cyclo(Arg-Gly-Asp-DPhe-NMeVal), par cyclisation d'un pentapeptide linéaire choisi parmi le groupe constitué de : H-Arg(Pbf) -Asp(OBzl) -DPhe-NMeVal-OH, H-Gly-Asp(OBzl) -DPhe- NMeVal-Arg (Pbf)-OH, H-Asp(OBzl) -DPhe-NMeVal-Arg (Pbf)-Gly-OH, H-DPhe-NMeVal- Arg (Pbf)-Gly-Asp (OBzl)-OH ou H-NMeVal-Arg-Arg (Pbf)-Gly-Asp (OBzl)-DPhe-OH; par dissociation ultérieure des groupes protecteurs et, éventuellement, par une autre conversion en sels physiologiquement acceptables.

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